Short communicationThe efficacy of artemisinin, artemether, and lumefantrine against Babesia gibsoni in vitro
Graphical abstract
The evaluation of the efficacy of combination drugs. Gray zone shows synergism, dark gray zone shows additive interaction, and white zone shows antagonism.
The combination artemisinin/lumefantrine against wild-type and atovaquone-resistant B. gibsoni showed synergism.
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Babesia in North America: An Update
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2020, Annual Reports in Medicinal ChemistryCitation Excerpt :Worryingly, three incidents of drug resistance to atovaquone/azithromycin (defined by parasite relapse after more than 28 days of antibabesial treatment) in immunocompromised patients with B. microti were reported.56 Recently, studies with artemether and lumefantrine in vitro showed a positive synergistic interaction of these compounds against B. gibsoni.57 Compounds that directly target the pathways of parasite DNA and RNA synthesis of B. gibsoni and B. bovis, such as mycophenolate mofetil, mizoribine, ribavirin, and 7-nitroindole, directly inhibit propagations of these parasites in vitro.
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2019, TalantaCitation Excerpt :To improve the pharmacological properties of artemisinin, semisynthetic analogs were developed such as dihydroartemisinin, artesunate, and artemether [2]. These artemisinin analogs prove to be highly active against malaria parasites and different cancer cell lines including leukemia and colon cancer [3,4]. Therefore, there is a need for developing fast and sensitive methods of detecting artemisinin without the requirement of sophisticated equipment.
Lumefantrine and o-choline – Parasite metabolism specific drug molecules inhibited in vitro growth of Theileria equi and Babesia caballi in MASP culture system
2019, Ticks and Tick-borne DiseasesCitation Excerpt :In the present study, lumefantrine was most effective in inhibiting in vitro T. equi and B. caballi growth with respective IC50 of 30.90 μM and 5.58 μM. This drug has been effective for inhibiting in vitro growth of P. falciparum and Babesia gibsoni at IC50 of 147.7 nM (Mungthin et al., 2010) and 480 nM (Iguchi et al., 2015), respectively. Further, the recrudescence of T. equi and B. caballi parasites was not observed in this study at more than 50 μM and 20 μM concentration of lumefantrine, respectively.
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2018, Veterinary ParasitologyCitation Excerpt :Buparvaquone's mode of action on piroplasms is probably comparable to atovaquone's and similarly to the mechanism of B. gibsoni resistance to atovaquone, point mutations in the Theileria annulata cytochorome b gene have been associated with resistance to buparvaquone treatment of bovine theileriosis in cattle (Sharifiyazdi et al., 2012; Mhadhbi et al., 2015). Several other antiprotozoal drugs such as phenamidine, pentamidine, parvaquone, artemisinin derivatives and antibiotics with some anti-protozoal activity such as doxycycline, minocycline, clindamycin, enrofloxacin and metronidazole have been evaluated for the treatment of canine babesiosis with various levels of efficacy (Wulansari et al., 2003; Matsuu et al., 2008; Lin and Huang, 2010; Lin et al., 2012; Iguchi et al., 2015). Phenamidine is administered to dogs at 15–20 mg/kg SC with an optional second administration after 48 h.